General Information of Target

Target ID LDTP01969
Target Name Transferrin receptor protein 1 (TFRC)
Gene Name TFRC
Gene ID 7037
Synonyms
Transferrin receptor protein 1; TR; TfR; TfR1; Trfr; T9; p90; CD antigen CD71) [Cleaved into: Transferrin receptor protein 1, serum form; sTfR)]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MMDQARSAFSNLFGGEPLSYTRFSLARQVDGDNSHVEMKLAVDEEENADNNTKANVTKPK
RCSGSICYGTIAVIVFFLIGFMIGYLGYCKGVEPKTECERLAGTESPVREEPGEDFPAAR
RLYWDDLKRKLSEKLDSTDFTGTIKLLNENSYVPREAGSQKDENLALYVENQFREFKLSK
VWRDQHFVKIQVKDSAQNSVIIVDKNGRLVYLVENPGGYVAYSKAATVTGKLVHANFGTK
KDFEDLYTPVNGSIVIVRAGKITFAEKVANAESLNAIGVLIYMDQTKFPIVNAELSFFGH
AHLGTGDPYTPGFPSFNHTQFPPSRSSGLPNIPVQTISRAAAEKLFGNMEGDCPSDWKTD
STCRMVTSESKNVKLTVSNVLKEIKILNIFGVIKGFVEPDHYVVVGAQRDAWGPGAAKSG
VGTALLLKLAQMFSDMVLKDGFQPSRSIIFASWSAGDFGSVGATEWLEGYLSSLHLKAFT
YINLDKAVLGTSNFKVSASPLLYTLIEKTMQNVKHPVTGQFLYQDSNWASKVEKLTLDNA
AFPFLAYSGIPAVSFCFCEDTDYPYLGTTMDTYKELIERIPELNKVARAAAEVAGQFVIK
LTHDVELNLDYERYNSQLLSFVRDLNQYRADIKEMGLSLQWLYSARGDFFRATSRLTTDF
GNAEKTDRFVMKKLNDRVMRVEYHFLSPYVSPKESPFRHVFWGSGSHTLPALLENLKLRK
QNNGAFNETLFRNQLALATWTIQGAANALSGDVWDIDNEF
Target Type
Clinical trial
Target Bioclass
Transporter and channel
Family
Peptidase M28 family, M28B subfamily
Subcellular location
Secreted; Cell membrane
Function
Cellular uptake of iron occurs via receptor-mediated endocytosis of ligand-occupied transferrin receptor into specialized endosomes. Endosomal acidification leads to iron release. The apotransferrin-receptor complex is then recycled to the cell surface with a return to neutral pH and the concomitant loss of affinity of apotransferrin for its receptor. Transferrin receptor is necessary for development of erythrocytes and the nervous system. A second ligand, the heditary hemochromatosis protein HFE, competes for binding with transferrin for an overlapping C-terminal binding site. Positively regulates T and B cell proliferation through iron uptake. Acts as a lipid sensor that regulates mitochondrial fusion by regulating activation of the JNK pathway. When dietary levels of stearate (C18:0) are low, promotes activation of the JNK pathway, resulting in HUWE1-mediated ubiquitination and subsequent degradation of the mitofusin MFN2 and inhibition of mitochondrial fusion. When dietary levels of stearate (C18:0) are high, TFRC stearoylation inhibits activation of the JNK pathway and thus degradation of the mitofusin MFN2.; (Microbial infection) Acts as a receptor for new-world arenaviruses: Guanarito, Junin and Machupo virus.
TTD ID
T33976
Uniprot ID
P02786
DrugMap ID
TT8MG4S
Ensemble ID
ENST00000360110.9
HGNC ID
HGNC:11763
ChEMBL ID
CHEMBL3712860

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 36 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
HDSF-alk
 Probe Info 
2.34  LDD0197  [2]
A-EBA
 Probe Info 
3.50  LDD0215  [3]
FBPP2
 Probe Info 
3.43  LDD0318  [4]
CHEMBL5175495
 Probe Info 
14.33  LDD0196  [5]
CY-1
 Probe Info 
100.00  LDD0243  [6]
CY4
 Probe Info 
100.00  LDD0244  [6]
N1
 Probe Info 
100.00  LDD0242  [6]
C-Sul
 Probe Info 
2.25  LDD0066  [7]
TH211
 Probe Info 
Y503(12.49); Y523(11.55); Y689(5.31)  LDD0257  [8]
YN-1
 Probe Info 
100.00  LDD0444  [9]
STPyne
 Probe Info 
K128(5.25); K180(5.90); K240(8.62); K261(6.68)  LDD0277  [10]
ONAyne
 Probe Info 
K58(9.82); K95(10.00)  LDD0275  [10]
OPA-S-S-alkyne
 Probe Info 
K358(1.48); K665(1.78); K180(2.39); K177(2.39)  LDD3494  [11]
P11
 Probe Info 
6.74  LDD0201  [12]
Alkylaryl probe 1
 Probe Info 
3.00  LDD0388  [13]
Alkylaryl probe 2
 Probe Info 
3.00  LDD0390  [13]
DBIA
 Probe Info 
C353(1.54)  LDD3312  [14]
THZ1-DTB
 Probe Info 
C558(1.09)  LDD0460  [15]
BTD
 Probe Info 
C363(2.14)  LDD1700  [16]
Johansson_61
 Probe Info 
_(20.00)  LDD1485  [17]
AHL-Pu-1
 Probe Info 
C353(2.03)  LDD0170  [18]
Alkyne-RA190
 Probe Info 
2.31  LDD0299  [19]
HHS-482
 Probe Info 
Y503(1.54)  LDD0285  [20]
HHS-475
 Probe Info 
Y683(0.50)  LDD0265  [21]
ATP probe
 Probe Info 
N.A.  LDD0199  [22]
4-Iodoacetamidophenylacetylene
 Probe Info 
N.A.  LDD0038  [23]
IA-alkyne
 Probe Info 
N.A.  LDD0036  [23]
Lodoacetamide azide
 Probe Info 
N.A.  LDD0037  [23]
NHS
 Probe Info 
K261(0.00); K693(0.00); K371(0.00)  LDD0010  [24]
SF
 Probe Info 
Y211(0.00); Y683(0.00); Y20(0.00)  LDD0028  [25]
1c-yne
 Probe Info 
K693(0.00); K418(0.00)  LDD0228  [26]
Acrolein
 Probe Info 
H603(0.00); C353(0.00); H515(0.00); H35(0.00)  LDD0217  [27]
Cinnamaldehyde
 Probe Info 
C363(0.00); C353(0.00)  LDD0220  [27]
Crotonaldehyde
 Probe Info 
C353(0.00); H186(0.00); C363(0.00); H234(0.00)  LDD0219  [27]
Methacrolein
 Probe Info 
C353(0.00); H234(0.00); C363(0.00)  LDD0218  [27]
HHS-465
 Probe Info 
N.A.  LDD2240  [28]
PAL-AfBPP Probe
Click To Hide/Show 40 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C036
 Probe Info 
5.46  LDD1736  [29]
C041
 Probe Info 
5.86  LDD1741  [29]
C044
 Probe Info 
27.47  LDD1743  [29]
C045
 Probe Info 
4.99  LDD1744  [29]
C073
 Probe Info 
5.98  LDD1769  [29]
C108
 Probe Info 
8.63  LDD1795  [29]
C115
 Probe Info 
9.99  LDD1802  [29]
C129
 Probe Info 
11.16  LDD1811  [29]
C147
 Probe Info 
6.87  LDD1829  [29]
C149
 Probe Info 
10.34  LDD1830  [29]
C160
 Probe Info 
8.75  LDD1840  [29]
C164
 Probe Info 
6.82  LDD1844  [29]
C170
 Probe Info 
21.41  LDD1850  [29]
C171
 Probe Info 
5.50  LDD1851  [29]
C186
 Probe Info 
9.71  LDD1864  [29]
C197
 Probe Info 
7.11  LDD1873  [29]
C205
 Probe Info 
5.78  LDD1880  [29]
C208
 Probe Info 
13.09  LDD1883  [29]
C221
 Probe Info 
7.52  LDD1895  [29]
C223
 Probe Info 
7.06  LDD1897  [29]
C237
 Probe Info 
9.25  LDD1910  [29]
C265
 Probe Info 
12.91  LDD1936  [29]
C281
 Probe Info 
10.06  LDD1951  [29]
C302
 Probe Info 
8.57  LDD1971  [29]
C310
 Probe Info 
29.45  LDD1977  [29]
C326
 Probe Info 
12.91  LDD1990  [29]
C334
 Probe Info 
5.62  LDD1997  [29]
C425
 Probe Info 
13.64  LDD2080  [29]
C429
 Probe Info 
14.62  LDD2084  [29]
FFF probe11
 Probe Info 
12.59  LDD0471  [30]
FFF probe12
 Probe Info 
18.84  LDD0473  [30]
FFF probe13
 Probe Info 
7.20  LDD0475  [30]
FFF probe14
 Probe Info 
13.61  LDD0477  [30]
FFF probe2
 Probe Info 
12.72  LDD0463  [30]
FFF probe3
 Probe Info 
20.00  LDD0464  [30]
FFF probe9
 Probe Info 
20.00  LDD0470  [30]
JN0003
 Probe Info 
6.26  LDD0469  [30]
Alk-rapa
 Probe Info 
7.45  LDD0213  [31]
DA-2
 Probe Info 
N.A.  LDD0070  [32]
STS-1
 Probe Info 
N.A.  LDD0068  [33]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0548  1-(4-(Benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)-2-nitroethan-1-one MDA-MB-231 C363(0.86)  LDD2142  [16]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C363(1.15)  LDD2112  [16]
 LDCM0502  1-(Cyanoacetyl)piperidine MDA-MB-231 C363(0.72)  LDD2095  [16]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C363(1.17)  LDD2130  [16]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C363(1.39); C353(0.98)  LDD2117  [16]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C363(1.80)  LDD2152  [16]
 LDCM0510  3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)-3-oxopropanenitrile MDA-MB-231 C363(0.54)  LDD2103  [16]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C363(0.38)  LDD2132  [16]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C363(0.64)  LDD2131  [16]
 LDCM0025  4SU-RNA DM93 C353(2.03)  LDD0170  [18]
 LDCM0214  AC1 HEK-293T C353(0.95)  LDD1507  [34]
 LDCM0215  AC10 HEK-293T C353(1.02)  LDD1508  [34]
 LDCM0226  AC11 HEK-293T C353(1.02)  LDD1509  [34]
 LDCM0237  AC12 HEK-293T C353(1.03)  LDD1510  [34]
 LDCM0259  AC14 HEK-293T C353(1.02)  LDD1512  [34]
 LDCM0270  AC15 HEK-293T C353(1.01)  LDD1513  [34]
 LDCM0276  AC17 HEK-293T C353(1.05)  LDD1515  [34]
 LDCM0277  AC18 HEK-293T C353(1.02)  LDD1516  [34]
 LDCM0278  AC19 HEK-293T C353(1.24)  LDD1517  [34]
 LDCM0279  AC2 HEK-293T C353(1.01)  LDD1518  [34]
 LDCM0280  AC20 HEK-293T C353(1.02)  LDD1519  [34]
 LDCM0281  AC21 HEK-293T C353(0.99)  LDD1520  [34]
 LDCM0282  AC22 HEK-293T C353(0.99)  LDD1521  [34]
 LDCM0283  AC23 HEK-293T C353(1.03)  LDD1522  [34]
 LDCM0284  AC24 HEK-293T C353(0.94)  LDD1523  [34]
 LDCM0285  AC25 HEK-293T C353(1.01)  LDD1524  [34]
 LDCM0286  AC26 HEK-293T C353(0.95)  LDD1525  [34]
 LDCM0287  AC27 HEK-293T C353(0.99)  LDD1526  [34]
 LDCM0288  AC28 HEK-293T C353(1.11)  LDD1527  [34]
 LDCM0289  AC29 HEK-293T C353(1.00)  LDD1528  [34]
 LDCM0290  AC3 HEK-293T C353(0.94)  LDD1529  [34]
 LDCM0291  AC30 HEK-293T C353(0.98)  LDD1530  [34]
 LDCM0292  AC31 HEK-293T C353(1.03)  LDD1531  [34]
 LDCM0293  AC32 HEK-293T C353(0.96)  LDD1532  [34]
 LDCM0294  AC33 HEK-293T C353(1.00)  LDD1533  [34]
 LDCM0295  AC34 HEK-293T C353(0.97)  LDD1534  [34]
 LDCM0296  AC35 HEK-293T C353(1.01)  LDD1535  [34]
 LDCM0297  AC36 HEK-293T C353(1.00)  LDD1536  [34]
 LDCM0298  AC37 HEK-293T C353(0.99)  LDD1537  [34]
 LDCM0299  AC38 HEK-293T C353(1.00)  LDD1538  [34]
 LDCM0300  AC39 HEK-293T C353(0.91)  LDD1539  [34]
 LDCM0301  AC4 HEK-293T C353(1.05)  LDD1540  [34]
 LDCM0302  AC40 HEK-293T C353(0.99)  LDD1541  [34]
 LDCM0303  AC41 HEK-293T C353(1.00)  LDD1542  [34]
 LDCM0304  AC42 HEK-293T C353(1.06)  LDD1543  [34]
 LDCM0305  AC43 HEK-293T C353(0.95)  LDD1544  [34]
 LDCM0306  AC44 HEK-293T C353(1.02)  LDD1545  [34]
 LDCM0307  AC45 HEK-293T C353(1.03)  LDD1546  [34]
 LDCM0308  AC46 HEK-293T C353(0.99)  LDD1547  [34]
 LDCM0309  AC47 HEK-293T C353(1.00)  LDD1548  [34]
 LDCM0310  AC48 HEK-293T C353(0.94)  LDD1549  [34]
 LDCM0311  AC49 HEK-293T C353(0.99)  LDD1550  [34]
 LDCM0312  AC5 HEK-293T C353(1.00)  LDD1551  [34]
 LDCM0313  AC50 HEK-293T C353(1.02)  LDD1552  [34]
 LDCM0314  AC51 HEK-293T C353(0.93)  LDD1553  [34]
 LDCM0315  AC52 HEK-293T C353(1.02)  LDD1554  [34]
 LDCM0316  AC53 HEK-293T C353(0.96)  LDD1555  [34]
 LDCM0317  AC54 HEK-293T C353(0.99)  LDD1556  [34]
 LDCM0318  AC55 HEK-293T C353(0.98)  LDD1557  [34]
 LDCM0319  AC56 HEK-293T C353(0.97)  LDD1558  [34]
 LDCM0320  AC57 HEK-293T C353(0.97)  LDD1559  [34]
 LDCM0321  AC58 HEK-293T C353(1.06)  LDD1560  [34]
 LDCM0322  AC59 HEK-293T C353(1.02)  LDD1561  [34]
 LDCM0323  AC6 HEK-293T C353(1.06)  LDD1562  [34]
 LDCM0324  AC60 HEK-293T C353(1.03)  LDD1563  [34]
 LDCM0325  AC61 HEK-293T C353(1.03)  LDD1564  [34]
 LDCM0326  AC62 HEK-293T C353(1.01)  LDD1565  [34]
 LDCM0327  AC63 HEK-293T C353(1.04)  LDD1566  [34]
 LDCM0328  AC64 HEK-293T C353(0.99)  LDD1567  [34]
 LDCM0334  AC7 HEK-293T C353(1.06)  LDD1568  [34]
 LDCM0345  AC8 HEK-293T C353(1.00)  LDD1569  [34]
 LDCM0545  Acetamide MDA-MB-231 C363(0.53)  LDD2138  [16]
 LDCM0520  AKOS000195272 MDA-MB-231 C363(1.45)  LDD2113  [16]
 LDCM0248  AKOS034007472 HEK-293T C353(1.00)  LDD1511  [34]
 LDCM0356  AKOS034007680 HEK-293T C353(0.97)  LDD1570  [34]
 LDCM0275  AKOS034007705 HEK-293T C353(0.97)  LDD1514  [34]
 LDCM0020  ARS-1620 HCC44 C353(1.04)  LDD2171  [35]
 LDCM0498  BS-3668 MDA-MB-231 C363(0.64)  LDD2091  [16]
 LDCM0088  C45 HEK-293T 6.74  LDD0201  [12]
 LDCM0108  Chloroacetamide HeLa C353(0.00); H401(0.00); H603(0.00); H234(0.00)  LDD0222  [27]
 LDCM0367  CL1 HEK-293T C353(1.07)  LDD1571  [34]
 LDCM0368  CL10 HEK-293T C353(1.05)  LDD1572  [34]
 LDCM0369  CL100 HEK-293T C353(1.06)  LDD1573  [34]
 LDCM0370  CL101 HEK-293T C353(1.07)  LDD1574  [34]
 LDCM0371  CL102 HEK-293T C353(1.00)  LDD1575  [34]
 LDCM0372  CL103 HEK-293T C353(0.97)  LDD1576  [34]
 LDCM0373  CL104 HEK-293T C353(0.97)  LDD1577  [34]
 LDCM0374  CL105 HEK-293T C353(1.02)  LDD1578  [34]
 LDCM0375  CL106 HEK-293T C353(1.03)  LDD1579  [34]
 LDCM0376  CL107 HEK-293T C353(0.94)  LDD1580  [34]
 LDCM0377  CL108 HEK-293T C353(1.06)  LDD1581  [34]
 LDCM0378  CL109 HEK-293T C353(0.98)  LDD1582  [34]
 LDCM0379  CL11 HEK-293T C353(1.15)  LDD1583  [34]
 LDCM0380  CL110 HEK-293T C353(0.99)  LDD1584  [34]
 LDCM0381  CL111 HEK-293T C353(1.01)  LDD1585  [34]
 LDCM0382  CL112 HEK-293T C353(1.02)  LDD1586  [34]
 LDCM0383  CL113 HEK-293T C353(1.02)  LDD1587  [34]
 LDCM0384  CL114 HEK-293T C353(1.06)  LDD1588  [34]
 LDCM0385  CL115 HEK-293T C353(0.95)  LDD1589  [34]
 LDCM0386  CL116 HEK-293T C353(1.06)  LDD1590  [34]
 LDCM0387  CL117 HEK-293T C353(1.04)  LDD1591  [34]
 LDCM0388  CL118 HEK-293T C353(1.05)  LDD1592  [34]
 LDCM0389  CL119 HEK-293T C353(1.03)  LDD1593  [34]
 LDCM0390  CL12 HEK-293T C353(1.05)  LDD1594  [34]
 LDCM0391  CL120 HEK-293T C353(1.08)  LDD1595  [34]
 LDCM0392  CL121 HEK-293T C353(1.00)  LDD1596  [34]
 LDCM0393  CL122 HEK-293T C353(1.04)  LDD1597  [34]
 LDCM0394  CL123 HEK-293T C353(1.01)  LDD1598  [34]
 LDCM0395  CL124 HEK-293T C353(1.03)  LDD1599  [34]
 LDCM0396  CL125 HEK-293T C353(1.02)  LDD1600  [34]
 LDCM0397  CL126 HEK-293T C353(0.98)  LDD1601  [34]
 LDCM0398  CL127 HEK-293T C353(1.05)  LDD1602  [34]
 LDCM0399  CL128 HEK-293T C353(1.06)  LDD1603  [34]
 LDCM0400  CL13 HEK-293T C353(1.06)  LDD1604  [34]
 LDCM0401  CL14 HEK-293T C353(1.02)  LDD1605  [34]
 LDCM0402  CL15 HEK-293T C353(0.99)  LDD1606  [34]
 LDCM0403  CL16 HEK-293T C353(1.04)  LDD1607  [34]
 LDCM0404  CL17 HEK-293T C353(1.05)  LDD1608  [34]
 LDCM0405  CL18 HEK-293T C353(1.07)  LDD1609  [34]
 LDCM0406  CL19 HEK-293T C353(0.98)  LDD1610  [34]
 LDCM0407  CL2 HEK-293T C353(1.02)  LDD1611  [34]
 LDCM0408  CL20 HEK-293T C353(1.07)  LDD1612  [34]
 LDCM0409  CL21 HEK-293T C353(1.14)  LDD1613  [34]
 LDCM0410  CL22 HEK-293T C353(1.12)  LDD1614  [34]
 LDCM0411  CL23 HEK-293T C353(1.06)  LDD1615  [34]
 LDCM0412  CL24 HEK-293T C353(1.04)  LDD1616  [34]
 LDCM0413  CL25 HEK-293T C353(0.98)  LDD1617  [34]
 LDCM0414  CL26 HEK-293T C353(0.99)  LDD1618  [34]
 LDCM0415  CL27 HEK-293T C353(0.99)  LDD1619  [34]
 LDCM0416  CL28 HEK-293T C353(1.06)  LDD1620  [34]
 LDCM0417  CL29 HEK-293T C353(0.99)  LDD1621  [34]
 LDCM0418  CL3 HEK-293T C353(0.93)  LDD1622  [34]
 LDCM0419  CL30 HEK-293T C353(1.05)  LDD1623  [34]
 LDCM0420  CL31 HEK-293T C353(0.97)  LDD1624  [34]
 LDCM0421  CL32 HEK-293T C353(1.05)  LDD1625  [34]
 LDCM0422  CL33 HEK-293T C353(1.21)  LDD1626  [34]
 LDCM0423  CL34 HEK-293T C353(1.04)  LDD1627  [34]
 LDCM0424  CL35 HEK-293T C353(1.08)  LDD1628  [34]
 LDCM0425  CL36 HEK-293T C353(1.03)  LDD1629  [34]
 LDCM0426  CL37 HEK-293T C353(0.95)  LDD1630  [34]
 LDCM0428  CL39 HEK-293T C353(1.00)  LDD1632  [34]
 LDCM0429  CL4 HEK-293T C353(1.07)  LDD1633  [34]
 LDCM0430  CL40 HEK-293T C353(1.05)  LDD1634  [34]
 LDCM0431  CL41 HEK-293T C353(0.96)  LDD1635  [34]
 LDCM0432  CL42 HEK-293T C353(1.00)  LDD1636  [34]
 LDCM0433  CL43 HEK-293T C353(0.99)  LDD1637  [34]
 LDCM0434  CL44 HEK-293T C353(1.10)  LDD1638  [34]
 LDCM0435  CL45 HEK-293T C353(1.17)  LDD1639  [34]
 LDCM0436  CL46 HEK-293T C353(1.05)  LDD1640  [34]
 LDCM0437  CL47 HEK-293T C353(1.10)  LDD1641  [34]
 LDCM0438  CL48 HEK-293T C353(1.08)  LDD1642  [34]
 LDCM0439  CL49 HEK-293T C353(1.01)  LDD1643  [34]
 LDCM0440  CL5 HEK-293T C353(0.96)  LDD1644  [34]
 LDCM0441  CL50 HEK-293T C353(0.98)  LDD1645  [34]
 LDCM0443  CL52 HEK-293T C353(1.04)  LDD1646  [34]
 LDCM0444  CL53 HEK-293T C353(0.93)  LDD1647  [34]
 LDCM0445  CL54 HEK-293T C353(1.01)  LDD1648  [34]
 LDCM0446  CL55 HEK-293T C353(1.02)  LDD1649  [34]
 LDCM0447  CL56 HEK-293T C353(1.13)  LDD1650  [34]
 LDCM0448  CL57 HEK-293T C353(1.23)  LDD1651  [34]
 LDCM0449  CL58 HEK-293T C353(1.07)  LDD1652  [34]
 LDCM0450  CL59 HEK-293T C353(1.07)  LDD1653  [34]
 LDCM0451  CL6 HEK-293T C353(1.07)  LDD1654  [34]
 LDCM0452  CL60 HEK-293T C353(1.07)  LDD1655  [34]
 LDCM0453  CL61 HEK-293T C353(0.97)  LDD1656  [34]
 LDCM0454  CL62 HEK-293T C353(1.00)  LDD1657  [34]
 LDCM0455  CL63 HEK-293T C353(1.00)  LDD1658  [34]
 LDCM0456  CL64 HEK-293T C353(1.08)  LDD1659  [34]
 LDCM0457  CL65 HEK-293T C353(0.97)  LDD1660  [34]
 LDCM0458  CL66 HEK-293T C353(1.04)  LDD1661  [34]
 LDCM0459  CL67 HEK-293T C353(1.07)  LDD1662  [34]
 LDCM0460  CL68 HEK-293T C353(1.09)  LDD1663  [34]
 LDCM0461  CL69 HEK-293T C353(1.10)  LDD1664  [34]
 LDCM0462  CL7 HEK-293T C353(0.98)  LDD1665  [34]
 LDCM0463  CL70 HEK-293T C353(1.06)  LDD1666  [34]
 LDCM0464  CL71 HEK-293T C353(1.05)  LDD1667  [34]
 LDCM0465  CL72 HEK-293T C353(1.02)  LDD1668  [34]
 LDCM0466  CL73 HEK-293T C353(1.00)  LDD1669  [34]
 LDCM0467  CL74 HEK-293T C353(1.00)  LDD1670  [34]
 LDCM0469  CL76 HEK-293T C353(1.04)  LDD1672  [34]
 LDCM0470  CL77 HEK-293T C353(1.04)  LDD1673  [34]
 LDCM0471  CL78 HEK-293T C353(1.07)  LDD1674  [34]
 LDCM0472  CL79 HEK-293T C353(0.96)  LDD1675  [34]
 LDCM0473  CL8 HEK-293T C353(1.18)  LDD1676  [34]
 LDCM0474  CL80 HEK-293T C353(1.03)  LDD1677  [34]
 LDCM0475  CL81 HEK-293T C353(1.09)  LDD1678  [34]
 LDCM0476  CL82 HEK-293T C353(1.06)  LDD1679  [34]
 LDCM0477  CL83 HEK-293T C353(1.08)  LDD1680  [34]
 LDCM0478  CL84 HEK-293T C353(0.94)  LDD1681  [34]
 LDCM0479  CL85 HEK-293T C353(1.04)  LDD1682  [34]
 LDCM0480  CL86 HEK-293T C353(0.95)  LDD1683  [34]
 LDCM0481  CL87 HEK-293T C353(0.98)  LDD1684  [34]
 LDCM0482  CL88 HEK-293T C353(1.07)  LDD1685  [34]
 LDCM0483  CL89 HEK-293T C353(0.99)  LDD1686  [34]
 LDCM0484  CL9 HEK-293T C353(1.13)  LDD1687  [34]
 LDCM0485  CL90 HEK-293T C353(1.10)  LDD1688  [34]
 LDCM0486  CL91 HEK-293T C353(0.97)  LDD1689  [34]
 LDCM0487  CL92 HEK-293T C353(1.12)  LDD1690  [34]
 LDCM0488  CL93 HEK-293T C353(1.09)  LDD1691  [34]
 LDCM0489  CL94 HEK-293T C353(1.07)  LDD1692  [34]
 LDCM0490  CL95 HEK-293T C353(1.29)  LDD1693  [34]
 LDCM0491  CL96 HEK-293T C353(1.05)  LDD1694  [34]
 LDCM0492  CL97 HEK-293T C353(1.02)  LDD1695  [34]
 LDCM0493  CL98 HEK-293T C353(1.03)  LDD1696  [34]
 LDCM0494  CL99 HEK-293T C353(1.02)  LDD1697  [34]
 LDCM0495  E2913 HEK-293T C353(0.98)  LDD1698  [34]
 LDCM0468  Fragment33 HEK-293T C353(0.99)  LDD1671  [34]
 LDCM0427  Fragment51 HEK-293T C353(1.02)  LDD1631  [34]
 LDCM0616  Fragment61 Jurkat _(6.83)  LDD1489  [17]
 LDCM0617  Fragment63-S Jurkat _(20.00)  LDD1490  [17]
 LDCM0569  Fragment7 Jurkat _(20.00)  LDD1485  [17]
 LDCM0117  HHS-0201 DM93 Y683(0.50)  LDD0265  [21]
 LDCM0118  HHS-0301 DM93 Y683(0.32)  LDD0266  [21]
 LDCM0119  HHS-0401 DM93 Y683(0.21)  LDD0267  [21]
 LDCM0120  HHS-0701 DM93 Y683(0.19)  LDD0268  [21]
 LDCM0107  IAA HeLa H401(0.00); C353(0.00); H515(0.00); H234(0.00)  LDD0221  [27]
 LDCM0123  JWB131 DM93 Y503(1.54)  LDD0285  [20]
 LDCM0124  JWB142 DM93 Y503(2.15)  LDD0286  [20]
 LDCM0125  JWB146 DM93 Y503(1.42)  LDD0287  [20]
 LDCM0126  JWB150 DM93 Y503(11.58)  LDD0288  [20]
 LDCM0127  JWB152 DM93 Y503(4.23)  LDD0289  [20]
 LDCM0128  JWB198 DM93 Y503(0.13)  LDD0290  [20]
 LDCM0129  JWB202 DM93 Y503(1.21)  LDD0291  [20]
 LDCM0130  JWB211 DM93 Y503(1.23)  LDD0292  [20]
 LDCM0022  KB02 HEK-293T C353(1.04)  LDD1492  [34]
 LDCM0023  KB03 HEK-293T C353(1.01)  LDD1497  [34]
 LDCM0024  KB05 HMCB C353(1.54)  LDD3312  [14]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C363(0.60)  LDD2102  [16]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C363(0.82)  LDD2121  [16]
 LDCM0109  NEM HeLa H603(0.00); H515(0.00); H401(0.00); C353(0.00)  LDD0223  [27]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C363(0.65)  LDD2089  [16]
 LDCM0497  Nucleophilic fragment 11b MDA-MB-231 C363(0.77)  LDD2090  [16]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C363(0.68)  LDD2092  [16]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C363(0.82)  LDD2093  [16]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C363(1.05)  LDD2094  [16]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C363(0.85)  LDD2097  [16]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C363(1.22)  LDD2099  [16]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C363(0.75)  LDD2100  [16]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C363(2.60)  LDD2101  [16]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C363(0.96)  LDD2104  [16]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C363(1.02)  LDD2105  [16]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C363(0.80)  LDD2106  [16]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C363(0.98)  LDD2107  [16]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C363(1.06)  LDD2108  [16]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C363(1.19)  LDD2109  [16]
 LDCM0517  Nucleophilic fragment 21b MDA-MB-231 C363(0.93)  LDD2110  [16]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C363(1.30)  LDD2111  [16]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C363(0.98)  LDD2114  [16]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C363(0.66)  LDD2115  [16]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C363(2.35)  LDD2119  [16]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C363(0.98)  LDD2120  [16]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C363(0.87)  LDD2123  [16]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C363(1.02)  LDD2125  [16]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C363(1.32)  LDD2127  [16]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C363(1.04)  LDD2128  [16]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C363(1.04)  LDD2129  [16]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C363(0.87)  LDD2133  [16]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C363(0.48)  LDD2134  [16]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C363(1.03)  LDD2135  [16]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C363(1.26); C353(1.46)  LDD2136  [16]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C363(1.37); C353(1.42)  LDD2137  [16]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C363(2.14)  LDD1700  [16]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C363(0.91)  LDD2140  [16]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C363(1.41)  LDD2143  [16]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C363(3.12)  LDD2144  [16]
 LDCM0551  Nucleophilic fragment 5b MDA-MB-231 C363(1.08)  LDD2145  [16]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C363(0.87)  LDD2146  [16]
 LDCM0553  Nucleophilic fragment 6b MDA-MB-231 C363(2.66)  LDD2147  [16]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C363(0.72)  LDD2148  [16]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C363(0.61)  LDD2150  [16]
 LDCM0559  Nucleophilic fragment 9b MDA-MB-231 C363(1.12)  LDD2153  [16]
 LDCM0099  Phenelzine MDA-MB-231 3.00  LDD0388  [13]
 LDCM0131  RA190 MM1.R 2.31  LDD0299  [19]
 LDCM0090  Rapamycin JHH-7 7.45  LDD0213  [31]
 LDCM0021  THZ1 HeLa S3 C558(1.09)  LDD0460  [15]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Ferritin heavy chain (FTH1) Ferritin family P02794
3-hydroxyisobutyrate dehydrogenase, mitochondrial (HIBADH) HIBADH-related family P31937
Glutathione S-transferase 3, mitochondrial (MGST3) MAPEG family O14880
ADP-ribosylation factor-like protein 13B (ARL13B) Arf family Q3SXY8
Transporter and channel
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Hepatic sodium/bile acid cotransporter (SLC10A1) Bile acid:sodium symporter (BASS) family Q14973
LHFPL tetraspan subfamily member 5 protein (LHFPL5) LHFP family Q8TAF8
Aquaporin-6 (AQP6) MIP/aquaporin (TC 1.A.8) family Q13520
Transferrin receptor protein 1 (TFRC) Peptidase M28 family P02786
Guided entry of tail-anchored proteins factor 1 (GET1) WRB/GET1 family O00258
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cyclic AMP-responsive element-binding protein 3-like protein 1 (CREB3L1) BZIP family Q96BA8
GPCR
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Probable G-protein coupled receptor 152 (GPR152) G-protein coupled receptor 1 family Q8TDT2
Immunoglobulin
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Hereditary hemochromatosis protein (HFE) MHC class I family Q30201
Other
Click To Hide/Show 10 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Albumin (ALB) ALB/AFP/VDB family P02768
Protein FAM209A (FAM209A) FAM209 family Q5JX71
Protein FAM210B, mitochondrial (FAM210B) FAM210 family Q96KR6
P antigen family member 1 (PAGE1) GAGE family O75459
RELT-like protein 2 (RELL2) RELT family Q8NC24
Regulator of microtubule dynamics protein 3 (RMDN3) RMDN family Q96TC7
Small glutamine-rich tetratricopeptide repeat-containing protein alpha (SGTA) SGT family O43765
Serotransferrin (TF) Transferrin family P02787
Ras association domain-containing protein 3 (RASSF3) . Q86WH2
SH3 domain-binding protein 4 (SH3BP4) . Q9P0V3

The Drug(s) Related To This Target

Approved
Click To Hide/Show 10 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Iron Small molecular drug DB01592
Ferric Cation . DB13949
Ferric Derisomaltose . DB15617
Ferrous Ascorbate . DB14490
Ferrous Fumarate . DB14491
Ferrous Gluconate . DB14488
Ferrous Glycine Sulfate . DB14501
Ferrous Succinate . DB14489
Ferrous Sulfate Anhydrous . DB13257
Tetraferric Tricitrate Decahydrate . DB14520
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Abbv-cx-2029 Antibody drug conjugate D58AMF

References

1 Labeling Preferences of Diazirines with Protein Biomolecules. J Am Chem Soc. 2021 May 5;143(17):6691-6700. doi: 10.1021/jacs.1c02509. Epub 2021 Apr 20.
Mass spectrometry data entry: PXD025140
2 Fatty Acyl Sulfonyl Fluoride as an Activity-Based Probe for Profiling Fatty Acid-Associated Proteins in Living Cells. Chembiochem. 2022 Feb 16;23(4):e202100628. doi: 10.1002/cbic.202100628. Epub 2021 Dec 30.
3 2-Ethynylbenzaldehyde-Based, Lysine-Targeting Irreversible Covalent Inhibitors for Protein Kinases and Nonkinases. J Am Chem Soc. 2023 Feb 12. doi: 10.1021/jacs.2c11595. Online ahead of print.
Mass spectrometry data entry: PXD037665
4 Tranylcypromine specificity for monoamine oxidase is limited by promiscuous protein labelling and lysosomal trapping. RSC Chem Biol. 2020 Aug 12;1(4):209-213. doi: 10.1039/d0cb00048e. eCollection 2020 Oct 1.
Mass spectrometry data entry: PXD018580
5 Charting the Chemical Space of Acrylamide-Based Inhibitors of zDHHC20. ACS Med Chem Lett. 2022 Sep 26;13(10):1648-1654. doi: 10.1021/acsmedchemlett.2c00336. eCollection 2022 Oct 13.
6 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
7 Low-Toxicity Sulfonium-Based Probes for Cysteine-Specific Profiling in Live Cells. Anal Chem. 2022 Mar 15;94(10):4366-4372. doi: 10.1021/acs.analchem.1c05129. Epub 2022 Mar 4.
8 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
9 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
10 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
11 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
12 Discovery of Potent and Selective Inhibitors against Protein-Derived Electrophilic Cofactors. J Am Chem Soc. 2022 Mar 30;144(12):5377-5388. doi: 10.1021/jacs.1c12748. Epub 2022 Mar 2.
13 Hydrazines as versatile chemical biology probes and drug-discovery tools for cofactor-dependent enzymes. bioRxiv, 2020-06.
14 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
15 A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification. J Am Chem Soc. 2019 Jan 9;141(1):191-203. doi: 10.1021/jacs.8b07911. Epub 2018 Dec 20.
16 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
17 Proteome-wide covalent ligand discovery in native biological systems. Nature. 2016 Jun 23;534(7608):570-4. doi: 10.1038/nature18002. Epub 2016 Jun 15.
18 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
19 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.
20 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
21 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
22 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
23 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
24 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
25 Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows. bioRxiv [Preprint]. 2023 Feb 18:2023.02.17.529022. doi: 10.1101/2023.02.17.529022.
Mass spectrometry data entry: PXD039931
26 Tunable Amine-Reactive Electrophiles for Selective Profiling of Lysine. Angew Chem Int Ed Engl. 2022 Jan 26;61(5):e202112107. doi: 10.1002/anie.202112107. Epub 2021 Dec 16.
27 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
28 Global profiling identifies a stress-responsive tyrosine site on EDC3 regulating biomolecular condensate formation. Cell Chem Biol. 2022 Dec 15;29(12):1709-1720.e7. doi: 10.1016/j.chembiol.2022.11.008. Epub 2022 Dec 6.
Mass spectrometry data entry: PXD038010
29 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
30 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.
31 Rapamycin targets STAT3 and impacts c-Myc to suppress tumor growth. Cell Chem Biol. 2022 Mar 17;29(3):373-385.e6. doi: 10.1016/j.chembiol.2021.10.006. Epub 2021 Oct 26.
32 Cell-based proteome profiling of potential dasatinib targets by use of affinity-based probes. J Am Chem Soc. 2012 Feb 15;134(6):3001-14. doi: 10.1021/ja208518u. Epub 2012 Feb 1.
33 Proteome profiling reveals potential cellular targets of staurosporine using a clickable cell-permeable probe. Chem Commun (Camb). 2011 Oct 28;47(40):11306-8. doi: 10.1039/c1cc14824a. Epub 2011 Sep 16.
34 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402
35 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.